A kind of finasteride lyotropic liquid crystal gel preparation precursor and preparation method thereof

Abstract

The invention belongs to the field of pharmaceutical preparations and discloses a finasteride lyotropic liquid crystal gel preparation precursor. The finasteride lyotropic liquid crystal gel preparation precursor comprises the following raw materials in percentage by mass: 45-80% of phospholipid, 10-50% of glyceride, 5-9% of a cosolvent and 0.1-6% of finasteride. The finasteride in the finasteridelyotropic liquid crystal gel preparation precursor disclosed by the invention is uniformly dispersed; the precursor is low in viscosity and can be used for injection; after entering a human body, theprecursor can act with water to form the lyotropic liquid crystal with an excellent drug sustained release effect; the biocompatibility is excellent, no systemic inflammatory response is caused, andtoxic and side effects of the medicine are avoided; the drug administration frequency can be decreased; the precursor is low in cost, simple in preparation method and capable of easily realizing industrialization; the precursor can be used for treating male hair loss and benign prostatic hyperplasia, so that an enlarged prostate is shrunk, and symptoms brought by urine flow and benign prostatic hyperplasia are improved.

Description

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a finasteride lyotropic liquid crystal gel preparation precursor and a preparation method thereof. Background technique

[0002] Finasteride is a 4-azasteroid that is a specific inhibitor of type II 5α-reductase, an intracellular enzyme involved in the metabolism of testosterone to the stronger dihydrotestosterone. Benign prostatic hyperplasia depends on the conversion of testosterone to dihydrotestosterone in the prostate. Finasteride is very effective in reducing DHT in the blood and in the prostate. Contain type II 5α-reductase in the hair follicle, and the hair follicle becomes less in the bald area scalp of male baldness patient, and dihydrotestosterone increases. Administration of finasteride can reduce the concentration of dihydrotestosterone in the scalp and serum of these patients. Men who are congenitally deficient in type II 5α-reductase do not...

Examples

preparation example Construction

[0043] The preparation method of the present invention is to use a high-speed stirrer, add phospholipids, glycerides and finasteride and mix them initially at a speed of 600-800rpm, then add a cosolvent and continue to stir for 20-30min at a speed of 1000-1500rpm, and then ultrasonicate while vacuuming After stirring for 20-30 minutes, the precursor of the finasteride lyotropic liquid crystal gel preparation is obtained. If necessary, the photosensitizer can be added together with the co-solvent, then stirred at high speed and vacuumed and ultrasonically stirred to obtain a finasteride lyotropic liquid crystal gel preparation precursor containing the photosensitizer. Finally, it was filled with nitrogen, sealed, and stored at -4°C.

[0044] The viscosity change test method of the finasteride lyotropic liquid crystal gel preparation precursor prepared by the present invention under different shear rates is as follows: use the Malvern Kinexus rotational rheometer to first measur...

Embodiment 1

[0051] This example provides a precursor of finasteride lyotropic liquid crystal gel preparation, which is prepared from the following raw materials in weight percentage: phosphatidylcholine 45%, glyceryl dioleate 49.9%, absolute ethanol 5%, Finasteride 0.1%.

[0052] The appearance of the product obtained in this example is a light yellow transparent solution, which shows that each raw material has good compatibility and is evenly mixed. There is no delamination phenomenon after storage at -4°C for 6 months and centrifugation treatment, indicating that the product has good storage stability.

[0053] The viscosity change graph of the finasteride lyotropic liquid crystal gel preparation precursor prepared in Example 1 at different shear rates is shown in figure 1 shown. It was found that when the viscosity of the prepared finasteride lyotropic liquid crystal gel preparation precursor reaches a certain shear rate, the shear viscosity remains unchanged and is not affected by t...

Embodiment 2

[0059] This example provides a precursor of finasteride lyotropic liquid crystal gel preparation, which is prepared from the following raw materials in weight percentage: phosphatidylcholine 80%, glyceryl dioleate 10%, peanut oil 9%, finasteride Andramine 1%.

[0060] The appearance of the product obtained in this example is a light yellow transparent solution, which shows that each raw material has good compatibility and is evenly mixed. There is no delamination phenomenon after storage at -4°C for 6 months and centrifugation treatment, indicating that the product has good storage stability.

[0061] The viscosity change diagram of the finasteride lyotropic liquid crystal gel preparation precursor under different shear rates in this embodiment is shown in figure 1 As shown, the shear stress has nothing to do with the shear speed, and its viscosity is constant, indicating that the precursor of the finasteride lyotropic liquid crystal gel preparation belongs to the plastic flu...

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a finasteride lyotropic liquid crystal gel preparation precursor and a preparation method thereof. Background technique

[0002] Finasteride is a 4-azasteroid that is a specific inhibitor of type II 5α-reductase, an intracellular enzyme involved in the metabolism of testosterone to the stronger dihydrotestosterone. Benign prostatic hyperplasia depends on the conversion of testosterone to dihydrotestosterone in the prostate. Finasteride is very effective in reducing DHT in the blood and in the prostate. Contain type II 5α-reductase in the hair follicle, and the hair follicle becomes less in the bald area scalp of male baldness patient, and dihydrotestosterone increases. Administration of finasteride can reduce the concentration of dihydrotestosterone in the scalp and serum of these patients. Men who are congenitally deficient in type II 5α-reductase do not...

Examples

preparation example Construction

[0043] The preparation method of the present invention is to use a high-speed stirrer, add phospholipids, glycerides and finasteride and mix them initially at a speed of 600-800rpm, then add a cosolvent and continue to stir for 20-30min at a speed of 1000-1500rpm, and then ultrasonicate while vacuuming After stirring for 20-30 minutes, the precursor of the finasteride lyotropic liquid crystal gel preparation is obtained. If necessary, the photosensitizer can be added together with the co-solvent, then stirred at high speed and vacuumed and ultrasonically stirred to obtain a finasteride lyotropic liquid crystal gel preparation precursor containing the photosensitizer. Finally, it was filled with nitrogen, sealed, and stored at -4°C.

[0044] The viscosity change test method of the finasteride lyotropic liquid crystal gel preparation precursor prepared by the present invention under different shear rates is as follows: use the Malvern Kinexus rotational rheometer to first measur...

Embodiment 1

[0051] This example provides a precursor of finasteride lyotropic liquid crystal gel preparation, which is prepared from the following raw materials in weight percentage: phosphatidylcholine 45%, glyceryl dioleate 49.9%, absolute ethanol 5%, Finasteride 0.1%.

[0052] The appearance of the product obtained in this example is a light yellow transparent solution, which shows that each raw material has good compatibility and is evenly mixed. There is no delamination phenomenon after storage at -4°C for 6 months and centrifugation treatment, indicating that the product has good storage stability.

[0053] The viscosity change graph of the finasteride lyotropic liquid crystal gel preparation precursor prepared in Example 1 at different shear rates is shown in figure 1 shown. It was found that when the viscosity of the prepared finasteride lyotropic liquid crystal gel preparation precursor reaches a certain shear rate, the shear viscosity remains unchanged and is not affected by t...

Embodiment 2

[0059] This example provides a precursor of finasteride lyotropic liquid crystal gel preparation, which is prepared from the following raw materials in weight percentage: phosphatidylcholine 80%, glyceryl dioleate 10%, peanut oil 9%, finasteride Andramine 1%.

[0060] The appearance of the product obtained in this example is a light yellow transparent solution, which shows that each raw material has good compatibility and is evenly mixed. There is no delamination phenomenon after storage at -4°C for 6 months and centrifugation treatment, indicating that the product has good storage stability.

[0061] The viscosity change diagram of the finasteride lyotropic liquid crystal gel preparation precursor under different shear rates in this embodiment is shown in figure 1 As shown, the shear stress has nothing to do with the shear speed, and its viscosity is constant, indicating that the precursor of the finasteride lyotropic liquid crystal gel preparation belongs to the plastic flu...

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